Delmopinol is a morpholino compound that has utility in the treatment of the oral cavity, in particular for the prevention and treatment of gingivitis and for the removal or inhibition of dental plaque. The compound and its manufacture are disclosed in U.S. Pat. No. 4,894,221.
Delmopinol Hydrochloride is used commonly in oral formulations, particularly mouth washes. However, delmopinol HCl is highly soluble in water and, when used in oral formulations, the delmopinol is removed from the oral surfaces (where it exerts its action) by the flow of saliva. Delmopinol HCl is so soluble that even in areas of the mouth with low saliva flow, it is only present for a relatively short time. Therefore, it is recommended that currently available products are held in the mouth for up to a minute, to achieve maximum efficacy. In addition, the concentration of delmopinol required for efficacy is high (0.2%) and contributes significantly to the cost of oral formulations.
There is a need for a formulation that provides delmopinol and related compounds in a form that will remain at oral surfaces for longer periods. Such a formulation will provide greater efficacy, at lower concentrations of delmopinol and/or when used for shorter periods of time, as a result of improved substantivity. In addition, the cost of the formulations should be reduced through achieving efficacy at a lower concentration of delmopinol.